The NF-kappaB/Rel signaling system is a paradigm for gene activation in response to inflammatory and menacing stimuli. A growing body of evidence provides a significant role of NF-kappaB for the onset of autoimmune diseases and different types of cancer. NF-kappaB is a drug target for the adjuvant therapy of these diseases. U.S. Pat. No. 6,878,735 discloses multi-substituted imidazolines as inhibitors or NF-κB. However, there remains a need for improved NF-κB inhibitors that have optimized therapeutic properties such as improved efficacy and reduced adverse drug reactions.